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Rhomboid protease inhibitors: Emerging tools and future therapeutics
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SYSNO ASEP 0469951 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Rhomboid protease inhibitors: Emerging tools and future therapeutics Author(s) Stříšovský, Kvido (UOCHB-X) RID, ORCID Source Title Seminars in Cell & Developmental Biology. - : Elsevier - ISSN 1084-9521
Roč. 60, Dec (2016), s. 52-62Number of pages 11 s. Language eng - English Country GB - United Kingdom Keywords rhomboid protease ; inhibitor ; disease ; mechanism ; substrate specificity Subject RIV CE - Biochemistry R&D Projects LK11206 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) LO1302 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) Institutional support UOCHB-X - RVO:61388963 UT WOS 000391077200008 EID SCOPUS 84994680422 DOI https://doi.org/10.1016/j.semcdb.2016.08.021 Annotation Rhomboid-family intramembrane serine proteases are evolutionarily widespread. Their functions in different organisms are gradually being uncovered and already suggest medical relevance for infectious diseases and cancer. In contrast to these advances, selective inhibitors that could serve as efficient tools for investigation of physiological functions of rhomboids, validation of their disease relevance or as templates for drug development are lacking. In this review I extract what is known about rhomboid protease mechanism and specificity, examine the currently used inhibitors, their mechanism of action and limitations, and conclude by proposing routes for future development of rhomboid protease inhibitors. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Jana Procházková, Tel.: 220 183 418 Year of Publishing 2017 Electronic address http://www.sciencedirect.com/science/article/pii/S1084952116302592
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